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AR011229A1 - ADENOSINE-DERIVED COMPOUNDS ANTAGONISTS IN THE AI ADENOSINE RECEPTOR, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN MEDICINE. - Google Patents

ADENOSINE-DERIVED COMPOUNDS ANTAGONISTS IN THE AI ADENOSINE RECEPTOR, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN MEDICINE.

Info

Publication number
AR011229A1
AR011229A1 ARP980105590A ARP980105590A AR011229A1 AR 011229 A1 AR011229 A1 AR 011229A1 AR P980105590 A ARP980105590 A AR P980105590A AR P980105590 A ARP980105590 A AR P980105590A AR 011229 A1 AR011229 A1 AR 011229A1
Authority
AR
Argentina
Prior art keywords
alkyl
ring
group
optionally substituted
adenosine
Prior art date
Application number
ARP980105590A
Other languages
Spanish (es)
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR011229A1 publication Critical patent/AR011229A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Un compuesto de la formula (I) el cual es un agonista en el receptor de la adenosina Al, en donde: R2 es alquilo con 1 a 3 átomos, halogeno ohidrogeno; R3 es un grupo alquilo recto o ramificado, fluorado, de 1-6 átomos de carbono; R1 es un grupo seleccionado de: (1) -(alq)n-(C3-7)-cicloalquilo,que incluyen el cicloalquilo con puentes, el grupo cicloalquilo que está substituido opcionalmente por uno o más de los substituyentes seleccionados deOH, halogeno, -(C1-3) alcoxi, en donde (alq) es alquileno con C1-3 y n es 0 o 1; (2) un grupo heterocíclico alifático de anillos de 4 a 6 elementos quecontienen al menos un heteroátomo seleccionado de O, N o S, substituido opcionalmente por uno o más substituyentes seleccionados del grupo queconsiste de -(C1-3)alquilo, -CO2-(C1-4)alquilo, -CO(C1-3alquilo), -S(=O)n-(C 1-3alquilo), - CONRaRb (en donde Ra y Rb son independientemente H o C1-3alquilo) o =O; en donde existe un átomo de azufre en el anillo heterocíclico, y el azufre está substituido opcionalmente por (=O)n, en donde n es 1 o 2; (3)alquilo con C1-12 recto o ramificado, que incluye opcionalmente uno o más O, S (=O)n (en donde n es 0, 1 o 2) o grupos N substituidos dentro de la cadena dealquilo substituido poruno o más de los siguientes grupos, fenilo, halogeno, hidroxi o NRaRb en donde Ra y Rb ambos son C1-3 alquilo o hidrogeno; (4) unanillo aromático bicíclico fusionado (formula (II), en donde B es un grupo aromático heterocíclico de 5 o 6 elementos que contiene 1 o más átomos de O, No S, en donde el anillo bicíclico está unido al átomo de nitrogeno de la formula (I) por medio de un átomo del anillo A y el anillo B está substituidoopcionalmente por -CO2-(C1-3alquilo); (5) un grupo fenilo substituido opcionalmente por uno o más substituyentes seleccionados de: halogeno, -SO3H,A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein: R2 is alkyl with 1 to 3 atoms, halogen or hydrogen; R3 is a fluorinated straight or branched alkyl group of 1-6 carbon atoms; R1 is a group selected from: (1) - (alk) n- (C3-7) -cycloalkyl, which include the bridged cycloalkyl, the cycloalkyl group which is optionally substituted by one or more of the substituents selected from OH, halogen, - (C1-3) alkoxy, where (alq) is C1-3 alkylene and n is 0 or 1; (2) a 4- to 6-membered ring aliphatic heterocyclic group containing at least one heteroatom selected from O, N or S, optionally substituted by one or more substituents selected from the group consisting of - (C1-3) alkyl, -CO2- (C1-4) alkyl, -CO (C1-3alkyl), -S (= O) n- (C 1-3alkyl), - CONRaRb (where Ra and Rb are independently H or C1-3alkyl) or = O; where there is a sulfur atom in the heterocyclic ring, and the sulfur is optionally substituted by (= O) n, where n is 1 or 2; (3) straight or branched C1-12 alkyl, optionally including one or more O, S (= O) n (where n is 0, 1 or 2) or substituted N groups within the alkyl chain substituted by one or more of the following groups, phenyl, halogen, hydroxy or NRaRb where Ra and Rb are both C1-3 alkyl or hydrogen; (4) a fused bicyclic aromatic ring (formula (II), where B is a 5- or 6-membered heterocyclic aromatic group containing 1 or more O, No S atoms, where the bicyclic ring is attached to the nitrogen atom of formula (I) by means of an atom of ring A and ring B is optionally substituted by -CO2- (C1-3alkyl); (5) a phenyl group optionally substituted by one or more substituents selected from: halogen, -SO3H,

ARP980105590A 1997-11-08 1998-11-05 ADENOSINE-DERIVED COMPOUNDS ANTAGONISTS IN THE AI ADENOSINE RECEPTOR, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN MEDICINE. AR011229A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9723589.9A GB9723589D0 (en) 1997-11-08 1997-11-08 Chemical compounds

Publications (1)

Publication Number Publication Date
AR011229A1 true AR011229A1 (en) 2000-08-02

Family

ID=10821760

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980105590A AR011229A1 (en) 1997-11-08 1998-11-05 ADENOSINE-DERIVED COMPOUNDS ANTAGONISTS IN THE AI ADENOSINE RECEPTOR, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN MEDICINE.

Country Status (29)

Country Link
US (1) US6455510B1 (en)
EP (2) EP1030857B1 (en)
JP (1) JP2001522857A (en)
KR (1) KR20010031875A (en)
CN (1) CN1285843A (en)
AP (1) AP2000001801A0 (en)
AR (1) AR011229A1 (en)
AT (1) ATE273990T1 (en)
AU (1) AU2048399A (en)
BR (1) BR9813976A (en)
CA (1) CA2309200A1 (en)
CO (1) CO5021135A1 (en)
DE (1) DE69825780T2 (en)
EA (1) EA200000392A1 (en)
EE (1) EE200000285A (en)
ES (1) ES2222621T3 (en)
GB (1) GB9723589D0 (en)
HR (1) HRP20000275A2 (en)
HU (1) HUP0004082A2 (en)
IL (1) IL135964A0 (en)
IS (1) IS5477A (en)
MA (1) MA26565A1 (en)
NO (1) NO20002361L (en)
PE (1) PE20000013A1 (en)
PL (1) PL340921A1 (en)
SK (1) SK6722000A3 (en)
TR (1) TR200002131T2 (en)
WO (1) WO1999024449A2 (en)
ZA (1) ZA9810125B (en)

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GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
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JP5006330B2 (en) 2005-10-21 2012-08-22 ノバルティス アーゲー Human antibodies against IL13 and therapeutic uses
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US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
EA201200260A1 (en) 2009-08-12 2012-09-28 Новартис Аг HETEROCYCLIC HYDRAZONES AND THEIR APPLICATION FOR THE TREATMENT OF CANCER AND INFLAMMATION
CN102573846B (en) 2009-08-17 2015-10-07 因特利凯公司 Heterocyclic compounds and their uses
MX2012002179A (en) 2009-08-20 2012-03-16 Novartis Ag Heterocyclic oxime compounds.
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Also Published As

Publication number Publication date
TR200002131T2 (en) 2001-01-22
GB9723589D0 (en) 1998-01-07
ZA9810125B (en) 2000-05-05
JP2001522857A (en) 2001-11-20
DE69825780D1 (en) 2004-09-23
HRP20000275A2 (en) 2000-12-31
NO20002361D0 (en) 2000-05-05
CN1285843A (en) 2001-02-28
PE20000013A1 (en) 2000-01-21
DE69825780T2 (en) 2005-01-13
BR9813976A (en) 2000-09-26
WO1999024449A3 (en) 1999-08-19
EP1030857A2 (en) 2000-08-30
PL340921A1 (en) 2001-03-12
NO20002361L (en) 2000-07-05
IS5477A (en) 2000-05-03
CA2309200A1 (en) 1999-05-20
KR20010031875A (en) 2001-04-16
ATE273990T1 (en) 2004-09-15
EP1457495A1 (en) 2004-09-15
HUP0004082A2 (en) 2001-04-28
MA26565A1 (en) 2004-12-20
CO5021135A1 (en) 2001-03-27
WO1999024449A2 (en) 1999-05-20
AU2048399A (en) 1999-05-31
US6455510B1 (en) 2002-09-24
SK6722000A3 (en) 2001-01-18
AP2000001801A0 (en) 2000-06-30
IL135964A0 (en) 2001-05-20
ES2222621T3 (en) 2005-02-01
EP1030857B1 (en) 2004-08-18
EA200000392A1 (en) 2000-12-25
EE200000285A (en) 2001-08-15

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